Deprecated: Implicit conversion from float 213.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Bioorg+Med+Chem+Lett 2015 ; 25 (21): 4961-9 Nephropedia Template TP
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Small cyclic agonists of iron regulatory hormone hepcidin #MMPMID25813158
Chua K; Fung E; Micewicz ED; Ganz T; Nemeth E; Ruchala P
Bioorg Med Chem Lett 2015[Nov]; 25 (21): 4961-9 PMID25813158show ga
Minihepcidins are in vitro and in vivo active mimetics of iron-regulatory hormone hepcidin. They contain various unusual amino acids including: N-substituted, ?-homo-, and D-amino acids with their combination depending on particular minihepcidin. In the current study, we sought to limit the use of unusual/more expensive amino acids derivatives by peptide cyclisation. Novel cyclic mimetics of hepcidin were synthesized and tested in vitro and showed activity at low nanomolar concentration. Nonetheless, the most active cyclic compound (mHS17) is approximately ten times less active than the parental minihepcidin PR73. Collectively, our findings suggest that cyclisation is viable approach in the synthesis of hepcidin mimetics.